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Efficient Synthesis and Anti-Tubercular Activity of a Series of Spirocycles: An Exercise in Open Science

Figure 2

Potential for the rapid synthesis of Spiros analogues via a common 2° amine intermediate 3.

(A) An existing oxa-Pictet–Spengler reaction can be used to form the spirocycle core (blue) as the 2° amine 3 [12]. (B) Strategy to diversify from the 2° core 3 to produce Spiros analogues (C) with variation at the piperidine nitrogen (red).

Figure 2

doi: https://doi.org/10.1371/journal.pone.0111782.g002